ArticleACS infectious diseases2017
Alkoxycarbonate Ester Prodrugs of Preclinical Drug Candidate ELQ-300 for Prophylaxis and Treatment of Malaria.
Article in ACS infectious diseases, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
30 citing papers in PubMed, 53 citations in OpenAlex.
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- Chemoprevention of malaria with long-acting oral and injectable drugs: an updated target product profile.Malaria journal · 2024Review
- Incorporation of an Isohexide Subunit into the Endochin-like Quinolone Scaffold.Molecules (Basel, Switzerland) · 2024Article
- 3-Position Biaryl Endochin-like Quinolones with Enhanced Antimalarial Performance.ACS infectious diseases · 2024Article
- Long-acting intramuscular injections of ELQ-331, an antimalarial agent.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2024Article
- Synthesis of Deuterated Endochin-Like Quinolones.Journal of labelled compounds & radiopharmaceuticals · 2024Article
- Susceptibility of Ugandan Plasmodium falciparum Isolates to the Antimalarial Drug Pipeline.Microbiology spectrum · 2023Article
- Quinolone: a versatile therapeutic compound class.Molecular diversity · 2023Review
- 7-ACS infectious diseases · 2023Article
- Structure-activity relationships ofExpert opinion on drug discovery · 2022Article
- Treatment of Human Babesiosis: Then and Now.Pathogens (Basel, Switzerland) · 2021Review
- A New Scalable Synthesis of ELQ-300, ELQ-316, and other Antiparasitic Quinolones.Organic process research & development · 2021Article
- Effective Therapy Targeting CytochromeAntimicrobial agents and chemotherapy · 2021Article
- Acridones Are Highly Potent Inhibitors ofACS infectious diseases · 2021Article
- Nanobiotechnological modules as molecular target tracker for the treatment and prevention of malaria: options and opportunity.Drug delivery and translational research · 2020Review
- Improving solubility and oral bioavailability of a novel antimalarial prodrug: comparing spray-dried dispersions with self-emulsifying drug delivery systems.Pharmaceutical development and technology · 2020Article
Corrections and comments
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Authors and funding
20 authors at 4 institutions in 1 country.
Funding
Abstract
ELQ-300 is a preclinical antimalarial drug candidate that is active against liver, blood, and transmission stages of Plasmodium falciparum. While ELQ-300 is highly effective when administered in a low multidose regimen, poor aqueous solubility and high crystallinity have hindered its clinical development. To overcome its challenging physiochemical properties, a number of bioreversible alkoxycarbonate ester prodrugs of ELQ-300 were synthesized. These bioreversible prodrugs are converted to ELQ-300 by host and parasite esterase action in the liver and bloodstream of the host. One such alkoxycarbonate prodrug, ELQ-331, is curative against Plasmodium yoelii with a single low dose of 3 mg/kg in a murine model of patent malaria infection. ELQ-331 is at least as fully protective as ELQ-300 in a murine malaria prophylaxis model when delivered 24 h before sporozoite inoculation at an oral dose of 1 mg/kg. Here, we show that ELQ-331 is a promising prodrug of ELQ-300 with improved physiochemical and metabolic properties and excellent potential for clinical formulation.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.